[Federal Register: July 7, 2003 (Volume 68, Number 129)]
[Notices]
[Page 40271-40273]
From the Federal Register Online via GPO Access [wais.access.gpo.gov]
[DOCID:fr07jy03-83]
-----------------------------------------------------------------------
DEPARTMENT OF HEALTH AND HUMAN SERVICES
National Institutes of Health
Government-Owned Inventions; Availability for Licensing
AGENCY: National Institutes of Health, Public Health Service, DHHS.
ACTION: Notice.
-----------------------------------------------------------------------
SUMMARY: The inventions listed below are owned by agencies of the U.S.
Government and are available for licensing in the U.S. in accordance
with 35 U.S.C. 207 to achieve expeditious commercialization of results
of federally-funded research and development. Foreign patent
applications are filed on selected inventions to extend market coverage
for companies and may also be available for licensing.
ADDRESSES: Licensing information and copies of the U.S. patent
applications listed below may be obtained by writing to the indicated
licensing contact at the Office of Technology Transfer, National
Institutes of Health, 6011 Executive Boulevard, Suite 325, Rockville,
Maryland 20852-3804; telephone: 301/496-7057; fax: 301/402-0220. A
signed Confidential Disclosure Agreement will
[[Page 40272]]
be required to receive copies of the patent applications.
Computer Based Model for the Identification and Characterization of
Noncompetitive Inhibitors of the Nicotinic Acetylcholine Receptors and
Related Ligand Gated Ion Channels
I. W. Wainer (NIA), K. Jozwiak (NIA), S. Ravichandran (SAIC-Frederick),
and J. R. Collins (SAIC-Frederick)
DHHS Reference No. E-158-2003/0 filed 11 Apr 2003
Licensing Contact: Cristina Thalhammer-Reyero; 301/435-4507;
thalhamc@mail.nih.gov.
NIH announces a method for the rapid determination and
characterization of noncompetitive inhibitors for nicotinic
acetylcholine receptors (nAChR) and other ligand gated ion channels, to
be used in drug discovery and development. Furthermore, inhibitors for
AChRs are described, which form a large and chemically heterogeneous
group of compounds that block the receptor. Inhibitors of AChRs affect
a large variety of physiological processes and many are used for
therapeutic purposes in different areas.
Classical methods for the identification and characterization of
noncompetitive inhibitors are time consuming and not effective in rapid
screening of chemical libraries for potential new drug candidates, nor
can they be routinely used in the new drug development process. This
invention describes the first computer-based model of the inner lumen
of a ligand gated ion channel, as well as unique, previously
unidentified and unexpected binding pockets. This method allows for
computer simulated structures of the members of chemical libraries to
be interacted with the computer-based model of the ligand gated channel
and the simulation used to predict and describe the pharmacological
importance of the interaction, and to screen for unexpected
interactions and toxicities of a drug candidate due to off-target
interactions.
Ligand gated ion channels are currently one of the largest targets
for drug discovery in the pharmaceutical industry. The Ligand Gated Ion
Channel superfamily is separated into the nicotinic receptor
superfamily (muscular and neuronal nicotinic, GABA-A and C, glycine and
5-HT3 receptors), the excitatory amino acid superfamily (glutamate,
aspartate and kainate receptors) and the ATP purinergic ligand gated
ion channels. These families only differ in the number of transmembrane
domains found in each subunit.
This work is partially described in Jozwiak et al., ``Displacement
and non-linear chromatographic techniques in the investigation of the
interaction of noncompetitive inhibitors with an immobilized
[alpha]3[]4 nicotinic acetylcholine
receptor liquid chromatographic stationary phase,'' Anal. Chem.
74:4618-4624, 2002.
HeadWave Clinical Coil Designed for Magnetic Resonance Elastography
David Moore and Seth Goldstein (NINDS)
DHHS Reference No. E-041-2003/0 filed 27 Mar 2003
Licensing Contact: Michael Shmilovich; 301/435-5019;
shmilovm@mail.nih.gov.
The invention is a novel device for measuring the elasticity of
cranially encased tissue. The device is a vibrator coil for use in
magnetic resonance elastography (MRE). The vibrator coil is applied to
the skull of a human patient using a transcranial Doppler monitoring
harness and applies mechanical and acoustic waves through the skull.
The propagation of the acoustic wave through brain tissue, coupled to
phase alteration of voxel isochromats in the presence of applied motion
encoding magnetic field gradients permits the measuring of intracranial
tissue elasticity.
HTLV-1 p30II and p12I Proteins as Therapeutic
Targets in HTLV-1 Infected Individuals
Genoveffa Franchini and Christophe Nicot (NCI)
DHHS Reference No. E-173-2001/0 filed 19 Aug 2002
Licensing Contact: Sally Hu; 301/435-5606; e-mail: hus@mail.nih.gov. The invention provides methods that use the HTLV-1 protein
p30II for identification of new drugs able to contain
expansion of HTLV-1 virus infected cells and methods of using the
identified compounds for treating patients with retroviral infection.
The present invention is based upon discovery that viral proteins
p30II and p12I are likely essential for the
survival of HTLV-1 infected cells. Working in concert these proteins
allow the replication of the infected cells while avoiding immune
recognition of the host. The data indicate that both p30II
and p12I can be employed as therapeutic targets in
containing replication of HTLV-1 infected cells, which in turn will
decrease an HTLV-1 infected patient's chance of developing
manifestations associated with HTLV-1 infection, e.g., adult T-cell
leukemia/lymphoma and tropical spastic paraperesis/HTLV-1 associated
myelopathy.
Methods and Compositions for Inhibiting HIV-Coreceptor Interactions
Oleg Chertov (NCI), Joost J. Oppenheim (NCI), Xin Chen (NCI), Connor
McGrath(NCI), Raymond C. Sowder II (NCI), Jacek Lubkowski (NCI),
Michele Wetzel (EM), and Thomas J. Rogers (EM)
DHHS Reference No. E-190-2000/0 filed 15 Feb 2001; PCT/US02/05063 filed
15 Feb 2002
Licensing Contact: Sally Hu; 301/435-5606; e-mail: hus@od.nih.gov.
This invention provides peptides that might be potent inhibitors of
HIV replication, in both macrophages and T lymphocytes. Specifically,
the inventors have identified peptides, from the HIV-1 gp120 envelope
protein, that share structural similarities with chemokines and are
shown to block ``docking'' interactions between the HIV-1 envelope
protein gp120 and chemokine receptors that function as ``coreceptors''
for HIV entry on the surface of target cells (macrophages and T
lymphocytes). The inventors synthesized two peptides (designated 15K
and 15D) based on this information and showed that both were effective
in competing with chemokines for binding to CCR5- and CXCR4-expressing
cells. These peptides efficiently inhibited infection of human monocyte
derived macrophages and peripheral blood mononuclear cells by different
strains of HIV. The synthesized peptides also inhibited monocyte
chemotaxis stimulated by the chemokine RANTES. Thus, these peptides and
other molecules based on their structure can be potentially used as
inhibitors of HIV. Moreover, these peptides could also have anti-
inflammatory and anti-tumor activity. Further, it has been determined
that these peptides are multi-tropic in their effects (blocking HIV
interactions with multiple co-receptors) for blocking both T cell
tropic (lymphotropic) and macrophage tropic (m-tropic) HIV strains.
3-D Video Image-Based Microscopic Precision Robotic Targeting
Jeffrey C. Smith (NINDS), James W. Nash (EM)
DHHS Reference No. E-162-2000/0 filed 22 Dec 2000
Licensing Contact: Michel Shmilovich; 301/435-5019;
shmilovm@mail.nih.gov.
The invention is a robotic software and hardware system that allows
a microscopic object such as a living biological cell to be targeted in
3-D
[[Page 40273]]
optical space for micromanipulation or probing (e.g., drug testing,
transgenic manipulation, nucleation/anucleation). The software permits
the selection of an object for targeting by a point and click operation
with a computer mouse, and performs the transforms between video pixel
space, optical space and micro-manipulator mechanical coordinate space
to translate the point and click operation into the precision targeting
movements of the micro-positioner. The object is viewed in real time
through a microscope system via a video output camera and displayed on
a computer terminal.
Applications include a variety of biological laboratory precision
tools such as positioning of microelectrodes for electrophysiological
recording from living cells, micro-injection and micro-manipulation of
cells and micro-delivery of pharmacological agents to cells for drug
testing and diagnostics.
The invention may also find application in microelectronics
fabrication.
Dated: June 27, 2003.
Steven M. Ferguson,
Acting Director, Division of Technology Development and Transfer,
Office of Technology Transfer, National Institutes of Health.
[FR Doc. 03-17077 Filed 7-3-03; 8:45 am]
BILLING CODE 4140-01-P